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16 条记录 (耗时 0.029 秒)

    Benzoyl Urea Derivatives
    4.
    发明申请
    Benzoyl Urea Derivatives 审中-公开

    公开(公告)号：US20090170901A1

    公开(公告)日：2009-07-02

    申请号：US11658788

    申请日：2005-07-21

    申请人： Istvan Borza ,  Gizella Bartané Szalai ,  Eva Bozo ,  Csilla Acsné Kiss ,  Csilla Horvath ,  Sandor Farkas ,  Jozsef Nagy ,  Sandor Kolok

    发明人： Istvan Borza ,  Gizella Bartané Szalai ,  Eva Bozo ,  Csilla Acsné Kiss ,  Csilla Horvath ,  Sandor Farkas ,  Jozsef Nagy ,  Sandor Kolok

    IPC分类号： A61K31/445 ,  C07D211/60 ,  A61P25/00

    CPC分类号： C07D295/215 ,  C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/34 ,  C07D211/46 ,  C07D401/12 ,  C07D413/12

    摘要： The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C1-C4 alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C1-C4 alkyl or C1-C4 alkoxycarbonyl group, or the neighboring X and Y groups optionally form together with one or more identical or different additional hetero atom and —CH═ and/or —CH2— groups an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably morpholine, pyrrole, pyrrolidine, oxo- or thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo- or thioxo-imidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo- or thioxo-oxazolidine, or 3-oxo-1,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl, hydroxy or optionally esterized carboxyl group, W is oxygen atom, as well as C1-C4 alkylene, C2-C4 alkenylene, aminocarbonyl, —NH—, —N(alkyl)-, —CH2O—, —CH2S—, —CH(OH)—, —OCH2— group, wherein the meaning of alkyl is a C1-C4 alkyl group—, when the dotted bonds () represent simple C—C bonds then U is hydroxy group or hydrogen atom or when W is C1-C4 alkylene or C2-C4 alkenylene group, then one of the dotted bonds () can represent a further double C—C bond and in this case U means an electron pair, which participate in the double bond and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor. Furthermore objects of the present invention are the pharmaceutical compositions containing new benzoyl urea derivatives of formula (I) or optical antipodes or racemates or the salts thereof as active ingredients and processes for producing these compounds and pharmaceutical compositions.

    Indole-2-carboxamidine derivatives as nmda receptor antago
    5.
    发明申请
    Indole-2-carboxamidine derivatives as nmda receptor antago 审中-公开
    吲哚-2-甲脒衍生物作为nmda受体拮抗剂

    公开(公告)号：US20090048303A1

    公开(公告)日：2009-02-19

    申请号：US11658787

    申请日：2005-07-21

    申请人： Istvan Borza ,  Csilla Horvath ,  Sandor Farkas ,  Jozsef Nagy ,  Sandor Kolok

    发明人： Istvan Borza ,  Csilla Horvath ,  Sandor Farkas ,  Jozsef Nagy ,  Sandor Kolok

    IPC分类号： A61K31/4439 ,  C07D209/14 ,  A61K31/404 ,  C07D401/02

    CPC分类号： C07D401/12 ,  C07D209/42 ,  C07D405/12

    摘要： The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C1-C4 alkyl, C1-C4 alkoxy group, or the neighboring V and Z groups in given case together with one or more identical or different additional hetero atom and —CH═ and/or —CH2— groups can form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably benzene, dioxolane ring, A, B and C independently are substituted carbon atom or one of them is nitrogen atom, and the salts thereof. Further objects of the invention are the processes for producing indole-2-carboxamidine derivatives of formula (I), and the pharmaceutical manufacture of medicaments containing these compounds, as well as the process of treatments with these compounds, which means administering to a mammal to be treated—including human—effective amount/amounts of indole-2-carboxamidine derivatives of formula (I) of the present invention as such or as medicament. The new indole-2-carboxamidine derivatives of formula (I) of the present invention are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.

    摘要翻译： 因此，本发明首先涉及式（I）的新的吲哚-2-甲脒衍生物，其中X的含义是氢或卤素原子，C1-C4烷基，C1-C4烷氧基，三氟甲基，Y，V和Z独立地 任选被卤素原子或卤原子取代的C 1 -C 4烷酰基氨基酰胺，任选被卤素原子或卤原子取代的C 1 -C 4烷酰胺基，三氟甲基，三氟甲氧基，C 1 -C 4烷基，C 1 -C 4 烷氧基或相邻的V和Z基团与一个或多个相同或不同的另外的杂原子和-CH-和/或-CH 2 - 基团可以形成任选取代的4-7元均 - 或杂环， 优选苯，二氧戊环，A，B和C独立地是取代的碳原子或其中一个是氮原子，及其盐。 本发明的另外的目的是制备式（I）的吲哚-2-甲脒衍生物和含有这些化合物的药物的药物制备方法以及用这些化合物处理的方法，这意味着给哺乳动物施用 包括人的有效量/本发明式（I）的吲哚-2-甲脒衍生物的量或作为药物。 本发明式（I）的新的吲哚-2-甲脒衍生物是NMDA受体的高效和选择性拮抗剂，而且大多数化合物是NMDA受体NR2B亚型的选择性拮抗剂。

    Amide derivatives as NMDA receptor antagonists
    7.
    发明授权
    Amide derivatives as NMDA receptor antagonists 失效
    酰胺衍生物作为NMDA受体拮抗剂

    公开(公告)号：US07375116B2

    公开(公告)日：2008-05-20

    申请号：US11025287

    申请日：2004-12-29

    申请人： Csilla Horvath ,  Sandor Farkas ,  György Domany ,  Istvan Borza ,  Gizella Bartane Szalai ,  Jozsef Nagy ,  Sandor Kolok

    发明人： Csilla Horvath ,  Sandor Farkas ,  György Domany ,  Istvan Borza ,  Gizella Bartane Szalai ,  Jozsef Nagy ,  Sandor Kolok

    IPC分类号： A61K31/445 ,  C07D401/06

    CPC分类号： C07D401/06 ,  A61K31/404 ,  A61K31/445 ,  A61K31/4523 ,  C07D209/42 ,  C07D211/16 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06 ,  C07D487/04

    摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.

    摘要翻译： 公开了具有NR2B选择性NMDA受体拮抗剂活性的化合物，其中相邻的R 1，R 2，R 3， R 4和R 4组合形成与吲哚核的苯环稠合的咪唑环，另外两个R 1，R 2， R 3和R 4基团是氢原子，R 5和R 6和它们之间的氮原子一起形成 被苯氧基，苯基 - （C 1 -C 4烷基），苯基 - （C 1 -C 4）烷基取代的饱和或不饱和的4-6元杂环， C 1 -C 4烷氧基），苯氧基 - （C 1 -C 4 -C 4烷基）或苯甲酰基，任选在 一个或多个卤素原子的芳香环，氰基或羟基，C 1 -C 4 -C 4烷基或C 1 -C 4 烷氧基，X是NH-，Y是-CH-基或其与酸或碱形成的药学上可接受的盐。